Antifungals

CDA-IN-4 (compound VS-24) is an inhibitor of chitin deacetylase (CDA). At a concentration of 100 μg/mL, CDA-IN-4 provides a protective effect of 61.2% against rice blast disease.

CDA-IN-3 (NCDI) is a chitin deacetylase (CDA) inhibitor with antiparasitic properties. It disrupts chitin metabolism in nematodes, increasing ROS levels within these organisms and causing cellular damage. CDA-IN-3 significantly inhibits all developmental stages of Caenorhabditis elegans and can be utilized in research focused on anti-infective applications.

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects,

Calpain Inhibitor-2, lipophilic, inhibits calpain; shows anti-proliferative effects on melanoma, PC-3 cells; blocks 80% DU-145 cell invasion.

Antifungal agent 17 showed good antifungal activity against B. cinerea (EC50: 2.86 μg/mL).

Isopyrazam, a plant protection product, exhibits potent antifungal activity. When applied to crops, it effectively inhibits the growth of various plant pathogenic fungi, significantly enhancing both the yield and quality of the crops. This compound demonstrates exceptional disease resistance capabilities in agricultural applications.

Complex III-IN-2 inhibits complex III, with antifungal EC50: 29.31 mg/L vs R. solani, 29.98 mg/L vs S. sclerotiorum.

Potent CHS inhibitor with an IC50 of 0.10 mM; exhibits broad-spectrum antifungal properties.

Antifungal agent 40 blocks C. albicans CYP51 in pocket II, hindering lanosterol demethylase and biofilm growth.

<p>SDH-IN-25 is an SDH inhibitor with an IC50 of 4.82 mg/L, demonstrating broad-spectrum and potent antifungal activity. By binding to SDH amino acid residues (TRP173, TYR58, and ARG43), it mimics the action mode of the commercial fungicide flutolanil. SDH-IN-25 induces changes in hyphal morphology, disrupts respiratory metabolism by binding to complex II, generates reactive oxygen species (ROS), and affects mitochondrial membrane potential (MMP) in hyphae. This compound is utilized in agricultural disease control research.</p>

AnCDA-IN-1 (Compound J075-4187) is an inhibitor of chitin deacetylase (CDA) exhibiting antifungal properties. It possesses an IC50 of 4.24 μM against A. nidulans AnCDA. The compound demonstrates a minimum inhibitory concentration (MIC) of 260 μg/mL and a minimum fungicidal concentration (MFC) of 520 μg/mL for food spoilage fungi and plant pathogenic fungi. AnCDA-IN-1 is applicable for research in the antifungal domain.

<p>WQ3810 TFA is an orally available fluoroquinolone with antimicrobial activity against Mycobacterium tuberculosis and inhibits the DNA rotamase activity of</p>

N'-(2-Fluorophenyl)pyrazine-2-carbohydrazide is a Ole1p desaturase inhibitor as well as antifungal agent [1].

Tenellin is a fungal metabolite that inhibits Mg2+-, Ca2+-, and Na+/K+-ATPase activities in erythrocytes. Tenellin is cytotoxic to Sf9 and Sf21 insect cells.

GW461484A is a small molecule inhibitor targeting Candida albicans Yck2, exhibiting an IC50 of 0.11 µM. It has a MIC80 of 12.5 µM against C. albicans. GW461484A shows potential for research into fungal diseases, including drug-resistant Candida infections.

A25822B is an antifungal agent.

Compound 2d (Antibacterial agent 188) serves as an antibacterial agent that suppresses the activity of dermatophytes [1].

<p>(Z)-Lanoconazole, an imidazole antifungal for dermatophytosis and onychomycosis, inhibits fungal ergosterol production.</p>

HSP90-IN-9: potent HSP90 inhibitor, dose-dependent fungicide, impedes biofilm/morphology with FLC, reverses FLC resistance.

Antifungal agent 13 demonstrates significant antifungal activity against Sclerotinia sclerotiorum, achieving an EC50 of 1.25 mg/L.

Yck2-IN-1 (Compound 2a) is an inhibitor of the fungus Candida albicans Yck2. It has an IC50 of approximately 80 nM for Yck2 and an MIC80 of 12.5 µM for C. albicans, demonstrating good metabolic stability [66% remaining in mouse liver microsomes]. In a mouse model with drug-resistant Candida, Yck2-IN-1 significantly reduced fungal load in the kidneys. Yck2-IN-1 shows potential for research in antifungal infection treatments.

Antifungal agent 100 (compound 3i) demonstrates notable antifungal activity, exhibiting an EC 50 of 0.33 mg/L against S. sclerotiorum. It also possesses an IC 50 value of 0.63 mg/mL targeting the Succinate dehydrogenase (SDH) of the same organism [1].

CYP51-IN-7 (compound 1g) is an analogue of Fluconazole and serves as an effective antifungal agent. It exhibits inhibitory activity against Microsporum gypseum and Candida albicans, with MIC80 values of 62.5 ng/mL and 250 ng/mL, respectively.

Antifungal agent 12 is a new fluconazole-like compound that exhibits good antifungal effects.

EGFR-IN-133 (Compound 24) serves as an inhibitor targeting various mutations of the EGFR, including the wild type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with respective IC50 values of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. The compound exhibits favorable pharmacokinetic properties and high oral bioavailability.

Chitin synthase inhibitor 8 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal effects that can be used in studies related to fungal infections

Complex III-IN-1 inhibits complex III, has antifungal properties, and an EC50 of 18.53 mg/L against S. sclerotiorum.

(3R,6S)-Bassiatin represents the enantiomeric form of the fungal metabolite known as bassiatin.

SARS-CoV-2 Mpro-IN-34 (Compound 26) acts as an inhibitor of SARS-CoV-2 Mpro with an IC50 of 6 nM. It also inhibits OC43 Mpro, demonstrating an IC50 of 33 nM. Furthermore, this compound exhibits antiviral activity in Vero E6 cells infected with SARS-CoV-2, with an EC50 of 0.103 μM.

CDA-IN-1 (Compound vs#2-1) is an inhibitor of chitin deacetylase (CDA) that exhibits antifungal activity. By inhibiting fungal CDA activity, it activates plant immune responses and leads to the accumulation of reactive oxygen species (ROS), hindering fungal growth. At a concentration of 100 μM, CDA-IN-1 achieves inhibition rates of 86.9% on P. xanthii's PxCDA1 and 74.5% on PxCDA2. CDA-IN-1 is applicable in research on fungal plant diseases, such as cucumber powdery mildew and tomato gray mold.

VNI is an effective inhibitor of CYP51. It suppresses sterol synthesis in Trypanosoma cruzi, exhibiting anti-Trypanosoma cruzi activity.

Chitin synthase inhibitor 12: potent CHS blocker (IC50: 0.16 mM), broad-spectrum antifungal, effective against resistant strains. Useful in IFI research.

<p>ATPase-IN-5 (Compound 11) is an antifungal Pma1p (H+ -ATPase) inhibitor (IC50 = 12.7 μM) that inhibits the growth of Candida albicans and Saccharomyces cerevisiae.</p>

Compound 9c, a chitin synthase inhibitor, has an IC50 of 0.37 nM and is useful for studying fungal infections.

Antifungalagent 127 (Compound 6c) is an antifungal agent with potent inhibitory activity against Botrytis cinerea and Rhizoctonia solani.

Ethaboxam is a β-tubulin inhibitor and antifungal agent used against oomycete pathogens.

RMG8-8 shows the excellent efficacy against C. neoformans (1.56 μg/mL).

HDAC-IN-87 (Compound XII6) is a non-selective HDAC inhibitor with pIC50 values of 6.9 for HDAC4 and 5.8 for HDAC6. It exhibits fungicidal activity against P. sorghi and P. pachyrhizi. The acute oral LD50 in both male and female rats is greater than 500 mg/kg.

Pyriofenone (IKF-309) is an aryl phenyl ketone fungicide predominantly used to control powdery mildew on crops such as cereals, rice, fruit trees, and vegetables. It exhibits moderate efficacy against rice blast disease. Pyriofenone functions through prevention, residue activity, treatment, rainfastness, translaminar action, and fumigation.

Antifungalagent 134 (Compound B13) is an antifungal agent effective against Botrytis cinerea, Alternaria solani, Fusarium graminearum, Rhizoctonia solani, Colletotrichum orbiculare, and Alternaria alternata with EC50 values of 3.24, 1.89, 1.70, 0.36, 4.27, and 1.50 μg/mL, respectively. It disrupts the fungal cell membranes and mitochondria, leading to substantial accumulation of reactive oxygen species (ROS). Additionally, Antifungalagent 134 exhibits significant herbicidal activity on field weeds such as Amaranthus retroflexus L and Abutilon theophrasti Medicus, and is applicable in crop disease and field weed research.

<p>D75-4590, a β-1,6-Glucan synthetase inhibitor, combats fungal infections by targeting cell walls.</p>

<p>Metabolite of voriconazole; sterol 14?-demethylase inhibitor</p>

Tetraconazole is an agent of pesticides.

2,7-Dihydroxynaphthalene is a useful organic compound for research related to life sciences. The catalog number is T67338 and the CAS number is 582-17-2.

Rhizocticin A is a potential inhibitor of threonine synthase.

<p>Amphotericin A is a polyene macrolide antibiotic, which is derived primarily from the soil bacterium *Streptomyces nodosus*. This compound functions by binding to ergosterol, an essential component of fungal cell membranes. This binding creates pores in the membrane, increasing its permeability and ultimately leading to cell death. Unlike its more widely used counterpart Amphotericin B, Amphotericin A is less frequently utilized but is critical in the study and understanding of antifungal activity.</p>

<p>1-(6-Amino-3,5-difluoro-2-pyridinyl)-7-[3-[3-[[1-(6-amino-3,5-difluoro-2-pyridinyl)-3-carboxy-8-chloro-6-fluoro-1,4-dihydro-4-oxo-7-quinolinyl]amino]-2-hydroxypropoxy]-1-azetidinyl]-8-chloro-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid is a fluoroquinolone antibiotic, engineered through synthetic chemistry. It is derived from chemical sources involving complex organic synthesis, highlighting its intricate molecular architecture. Its mode of action is distinctive, as it inhibits bacterial DNA gyrase and topoisomerase IV, enzymes crucial for DNA replication and transcription. This interference with bacterial DNA processes results in bactericidal effects, effectively eliminating susceptible bacterial strains.</p>